ArticleThe Biochemical journal2006
Modelling insecticide-binding sites in the voltage-gated sodium channel.
Article in The Biochemical journal, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 121 papers.
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Who cites it
121 citing papers in PubMed, 282 citations in OpenAlex.
- Mutations M918T, M918L, and L1014F impair pyrethroid binding and alter gating of the Megalurothrips usitatus sodium channel.Pest management science · 2026Article
- A genome sequence and efficient CRISPR/Cas9 gene editing tools for the solanaceous specialist pest Tetranychus evansi.Insect biochemistry and molecular biology · 2026Article
- Emerging and regionally novel voltage-gated sodium channel mutations associated with pyrethroid resistance and altered binding affinity in Aedes albopictus (Skuse) from Northern Peninsular Malaysia.Parasites & vectors · 2026Article
- Presence of localized elevated metabolic enzymes and kdr mutations in the voltage-gated sodium channel gene indicate early evidence of resistance of Phlebotomus argentipes to alpha-cypermethrin in Bihar, India.Parasites & vectors · 2026Article
- Whole-Genome Resequencing of the VGSC Reveals the Evolutionary Mechanism of Pesticide Resistance inInternational journal of molecular sciences · 2026Article
- Fine-scale spatio-temporal dynamics ofCurrent research in parasitology & vector-borne diseases · 2026Article
- Differential effects of dual and synergist-based insecticide-treated bed nets on pyrethroid resistance and L995F/S knockdown resistance mutation dynamics in Anopheles gambiae s.l. populations in south-western Burkina Faso.Parasites & vectors · 2025Article
- Pyrethroid and organochlorine susceptibility in Aedes aegypti populations from eastern black sea region, Türkiye: traces in the kdr gene region of the species origin.Parasitology research · 2025Article
- Molecular characterization of invasive Aedes albopictus (Diptera: Culicidae) populations in northwest Iran: Insights into origin, insecticide resistance, and Wolbachia infection.Parasites & vectors · 2025Article
- Pyrethroid resistance in Aedes aegypti: genetic mechanisms worldwide, and recommendations for effective vector control.Parasites & vectors · 2025Review
- Global distribution and impact of knockdown resistance mutations in Aedes aegypti on pyrethroid resistance.Parasites & vectors · 2025Review
- An atlas of positive selection in the genomes of major malaria vectors.bioRxiv : the preprint server for biology · 2025Article
- Response of Amblyseius swirskii to deltamethrin.Pest management science · 2025Article
- A unique mechanism of transfluthrin action revealed by mapping its binding sites in the mosquito sodium channel.Insect biochemistry and molecular biology · 2024Article
- Assessing pyrethroid resistance in Aedes aegypti from Cordoba Colombia: Implications of kdr mutations.PloS one · 2024Article
- Pyrethrins and Pyrethroids: A Comprehensive Review of Natural Occurring Compounds and Their Synthetic Derivatives.Plants (Basel, Switzerland) · 2023Review
- Knockdown resistance mutations are common and widely distributed in Xenopsylla cheopis fleas that transmit plague in Madagascar.PLoS neglected tropical diseases · 2023Article
- Pyrethroid-treated bed nets impair blood feeding performance in insecticide resistant mosquitoes.Scientific reports · 2023Article
- Article
- Contrasting Patterns ofMicroorganisms · 2023Article
61 more citing papers are in PubMed but not listed here.
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
A homology model of the housefly voltage-gated sodium channel was developed to predict the location of binding sites for the insecticides fenvalerate, a synthetic pyrethroid, and DDT an early generation organochlorine. The model successfully addresses the state-dependent affinity of pyrethroid insecticides, their mechanism of action and the role of mutations in the channel that are known to confer insecticide resistance. The sodium channel was modelled in an open conformation with the insecticide-binding site located in a hydrophobic cavity delimited by the domain II S4-S5 linker and the IIS5 and IIIS6 helices. The binding cavity is predicted to be accessible to the lipid bilayer and therefore to lipid-soluble insecticides. The binding of insecticides and the consequent formation of binding contacts across different channel elements could stabilize the channel when in an open state, which is consistent with the prolonged sodium tail currents induced by pyrethroids and DDT. In the closed state, the predicted alternative positioning of the domain II S4-S5 linker would result in disruption of pyrethroid-binding contacts, consistent with the observation that pyrethroids have their highest affinity for the open channel. The model also predicts a key role for the IIS5 and IIIS6 helices in insecticide binding. Some of the residues on the helices that form the putative binding contacts are not conserved between arthropod and non-arthropod species, which is consistent with their contribution to insecticide species selectivity. Additional binding contacts on the II S4-S5 linker can explain the higher potency of pyrethroid insecticides compared with DDT.
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